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参考中草药中某些抑菌成分的结构,设计出一种环取代苯乙醇衍生物——AF821作为化学合成抗真菌药物。本文报道了它的三条合成路线。并测定了它的急性毒性LD_(50)。抗菌研究结果表明,AF821在试管内对供试的十三种真菌均有不同程度的抗菌活性。对其中丝状真菌活性较强,如对石膏样毛癣菌的MIC为12.5μg/ml。对豚鼠实验性体癣也有一定治疗作用。经AF821作用后的真菌细胞,在电镜下可见膜系统呈破坏性改变,主要为细胞膜、线粒体膜和核膜的损伤。
With reference to the structure of some antibacterial components in Chinese herbal medicine, a ring substituted phenyl ethanol derivative (AF821) was designed as a chemical synthetic antifungal agent. This article reports its three synthetic routes. And its acute toxicity LD_ (50) was measured. The results of antibacterial study showed that AF821 had different degrees of antibacterial activities on the tested 13 fungi in vitro. Of which filamentous fungi activity is strong, such as Trichophyton mentagrophytes MIC 12.5μg / ml. Guinea pig experimental body tinea also have a therapeutic effect. After the fungal cells treated with AF821, the membrane system showed a destructive change under electron microscope, mainly the damage of cell membrane, mitochondrial membrane and nuclear membrane.